Field of the Invention
The invention relates to a field of novel compounds which have antineoplastic activity. More specifically, the invention relates to substituted 1,2,3-triazoles which have antineoplastic activity, a pharmaceutical composition including the same, and a method of treating a cancer disease in an individual.
Description of Related Art
Cancer, also known as a malignant tumor or malignant neoplasm, is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body, and remains one of the most important unmet medical challenges to mankind Cancer can be treated by surgery, chemotherapy, radiation therapy, hormonal therapy, and targeted therapy (including immunotherapy such as monoclonal antibody therapy), or any combination of these approaches. The choice of therapy depends upon the location and grade of the tumor and the stage of the disease, as well as the general state of the patient(performance status).
Among these approaches, chemotherapy is widely used for all types of cancers, in particular for those inoperable or with metastatic characteristics. Although a variety of chemotherapeutic compounds are used in clinics, tumors and their metastasis become refractory to chemotherapy when the tumor cells develop the ability of multidrug resistance. In some cases, the tumors are inherently resistant to some classes of chemotherapeutic agents. In other cases, the acquired resistance against chemotherapeutic agents is developed during the chemotherapeutic intervention.
Therefore, there remain significant limitations to the efficacy of available chemotherapeutic compounds in treating different classes of tumors, and thus there remains a need for new chemotherapeutic agents.
A triazole (Htrz) refers to either one of a pair of isomeric chemical compounds with molecular formula C2H3N3, having a five-membered ring of two carbon atoms and three nitrogen atoms. The five membered triazole ring exists in two tautomeric forms i.e. 1,2,3-triazole and 1,2,4-triazole. Both 1,2,3-triazole and 1,2,4-triazole and their derivatives are of great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities such as antiviral, antibacterial, antifungal, antituberculosis, anticonvulsant, antidepressant, anti-inflammatory, anticancer activities, etc. They have been reported to be inhibitors of glycogen synthase kinase-3, antagonists of GABA receptors, agonists of muscarine receptors, neuroleptic agent, and these compounds also show anti-HIV-1, cytotoxic, antihistaminic, and antiproliferative activities.
Thus, the design and synthesis of novel triazole derivatives are the prospective direction of medicinal chemistry for the scientists working in this field.
Based on common technical knowledge in the art, the compound may change greatly in stereostructure, spatial effect and electronic effect when the types and number of the substitutes and the substituted atomic species are different, thereby generating a great impact on the physicochemical property and pharmaceutical active thereof Thus, herein we describe the synthesis and anticancer activity of new substituted 1,2,3-triazoles which types and number of the substitutes thereof are different form existing substituted 1,2,3-triazoles.